Synthesis and biological evaluation of 2-(phenyl)-3H-benzo[d]imidazole-5-carboxylic acids and its methyl esters as potent anti-breast cancer agents

A series of novel substituted 2-(phenyl)-3H-benzo[d]imidazole-5-carboxylic acids (1a-1j) and its methyl esters (2a-2f) were synthesized and examined for their antiproliferative effects against three breast cancer cell lines (MDA-MB231, MDA-MB468 and MCF7) in vitro. Most of the compounds exhibited comparable or greater antiproliferative effects than the reference compound cisplatin. Compound 2e bearing 5-fluoro-2-hydroxyphenyl substituent was found to be the most active derivative of the series with GI50 values of 6.23, 4.09 and 0.18 μM against MDA-MB468, MDA-MB231 and MCF7 breast cancer cell lines, respectively. Our findings described here exemplify the usefulness of the title compounds as a lead for the development of more effective cancer therapeutics for the treatment of breast cancer.